The nonsteroidal anti-inflammatory drug (NSAID)group contains a large number of drugs. There are morethan 70 drugs in this category, with new drugs continually becoming available. Some texts include the salicy-lates in the NSAID group, whereas others do not.Although the chemical and physiologic effects are similar,The NSAIDs are another typeof nonnarcotic analgesic.
ACTIONS
The NSAIDs are so named because they do not belong to the steroid group of drugs and thus do not possess the adverse reactions associated with the steroid and yet they have anti-inflammatory effects.In addition, NSAIDs have analgesic and antipyretic properties. Although the exact mechanisms of actions
are not known, the NSAIDs are thought to act by inhibiting prostaglandin (a group of naturally occur-ring fatty acids that act within the body to regulate acid secretion of the stomach, regulate body temperature and platelet aggregation, and control inflammation) synthesis by inhibiting the action of the enzyme cyclooxyge
nase, the enzyme responsible for prostaglandin synthesis. The NSAIDs act to inhibit the activity of two related enzymes:
1. cycloo1xygenase-1 (COX-1), the enzyme that helps to maintain the stomach lining; and
2. cyclooxygenase-2 (COX-2), the enzyme that
triggers pain and inflammation.
The anti-inflammatory effects of the NSAIDs are carried out by inhibition of COX-2. The gastrointestinal adverse reactions are caused by inhibition of COX
1. The newer NSAIDs (celecoxib and rofecoxib) appear to work by specifically inhibiting the COX-2
enzyme, without inhibiting the COX-1 enzyme.Celecoxib and rofecoxib relieve pain and inflamma-tion with less potential for gastrointestinal adverse reactions. The traditional NSAIDs, such as ibuprofen and naproxen, are thought to regulate the pain and inflammation by blocking COX-2. Unlike celecoxib and rofecoxib, these drugs also inhibit COX-1, the enzyme that helps maintain the lining of the stomach. This inhibition of COX-1 causes the unwanted gastrointestinal reactions, such as stomach irritation and ulcers.
USES
The NSAIDs have a variety of uses that vary depending on the drug selected. NSAIDs are used for the following conditions:
• Relief of signs and symptoms of osteoarthritis,rheumatoid arthritis, and other musculoskeletal disorders
• Mild to moderate pain relief
• Primary dysmenorrhea
• Fever reduction
ADVERSE REACTIONS
Many adverse reactions are associated with the use of the NSAIDs. However, many patients take these drugs and experience few, if any, side effects. Some of the adverse reactions associated with the use of these drugs are listed here.
• Gastrointestinal tract nausea, vomiting, diarrhea, constipation, epigastric pain, indigestion,abdominal distress or discomfort, intestinal ulceration, stomatitis, jaundice, bloating, anorexia, and dry mouth
• Central nervous system dizziness, anxiety, lightheadedness, vertigo, headache, drowsiness, insomnia, confusion, depression, and psychic disturbances
• Cardiovascular—congestive heart failure, decreaseor increase in blood pressure, and cardiac arrhythmias
• Renal—hematuria, cystitis, elevated blood urea nitrogen, polyuria, dysuria, oliguria, and acute renal failure in those with impaired renal function
• Special senses—visual disturbances, blurred or diminished vision, diplopia, swollen or irritated eyes, photophobia, reversible loss of color vision,tinnitus, taste change, and rhinitis
• Hematologic—neutropenia, eosinophilia, leukopenia, pancytopenia, thrombocytopenia, agranulocytosis, and aplastic anemia
• Skin—rash, erythema, irritation, skin eruptions,exfoliative dermatitis, Stevens-Johnson syndrome,ecchymosis, and purpura
• Metabolic/endocrinologic—decreased appetite,weight increase or decrease, hyperglycemia, hypoglycemia, flushing, sweating, menstrual disorders,and vaginal bleeding
• Other—thirst, fever, chills, and vaginitis
CONTRAINDICATIONS, PRECAUTIONS,
AND INTERACTIONS
The NSAIDs are contraindicated in patients with known hypersensitivity. There is a cross-sensitivity to
other NSAIDs. Therefore, if a patient is allergic to one NSAID, there is an increased risk of an allergic reaction with any other NSAID. Hypersensitivity to aspirin is a contraindication for all NSAIDs. In general, the NSAIDs are contraindicated during the third trimester of pregnancy and during lactation.
The NSAIDs are used cautiously in patients with bleeding disorders, renal disease, cardiovascular disease, or hepatic impairment and in the elderly. There is an increased risk of ulcer formation in patients older
than 65 years. Most NSAIDs are classified as Pregnancy Category B. In general, the NSAIDs are
used with extreme caution during pregnancy, especially in large doses or during the third trimester (see
above).
The NSAIDs prolong bleeding time and increase the effects of anticoagulants, lithium, cyclosporine, and the
hydantoins. These drugs may decrease the effects of diuretics or antihypertensive drugs. Long-term use of
the NSAIDs with acetaminophen may increase the risk of renal impairment.
COMMON ADVERSE REACTIONS
OF SELECT NSAIDs
Celecoxib
The most common adverse reactions seen with cele-coxib include dyspepsia, abdominal pain, diarrhea, nau-sea, and headache. Like other NSAIDs, celecoxib may compromise renal function. Elevation of aminotrans-ferase levels also occurs.
Ibuprofen
This drug is available to individuals as an over-the-counter drug and may be purchased without a prescrip-tion. The drug is used in children with juvenile arthritis and for fever reduction in children 6 months to 12 years.
Common adverse reactions seen with ibuprofen include headache, dizziness, somnolence, nausea, dyspepsia, gas-trointestinal pain, and rash.
Naproxen
Common adverse reactions seen with naproxen include headache, vertigo (dizziness), somnolence, insomnia,nausea, dyspepsia, gastrointestinal pain, and rash.
Rofecoxib
Common adverse reactions seen with rofecoxib includeheadache, dizziness, somnolence, insomnia, dyspnea,hemoptysis, and rash.
CONTRAINDICATIONS, PRECAUTIONS
AND INTERACTIONS
Celecoxib
Celecoxib is contraindicated in patients who are allergic to the drug itself, the sulfonamides, other NSAIDs, or aspirin; it also is contraindicated during pregnancy (Category C) and lactation.
The drug is used cautiously in patients with a history of peptic ulcer, individuals older than 60 years, and those taking an anticoagulant or steroids. In rare instances, serious stomach problems such as bleeding can occur without warning. When celecoxib is given with the anticoagulants, there is an increased risk for
bleeding.
Ibuprofen
Ibuprofen is contraindicated in individuals who are allergic to the drug or other NSAIDs; those who have hypertension, peptic ulceration, or gastrointestinal bleeding; and during pregnancy (Category B) and lacta-tion. The drug is used cautiously in patients with renal or liver dysfunction. When ibuprofen is used with
lithium, there is an increased risk of lithium toxicity. A decreased effect of the diuretic may occur when admin-istered with ibuprofen.When ibuprofen is administered with the beta-adrenergic blocking drugs there is a risk for a decrease in the antihypertensive effect of the beta-adrenergic blocking drug.
Naproxen
Naproxen is contraindicated in patients who are allergic to the drug or other NSAIDs and during pregnancy (Category B) and lactation. The drug is used cautiously in patients with asthma, hypertension, cardiac problems, peptic ulcer disease, and impaired liver or kidney function. Like ibuprofen, naproxen increases the risk of lithium toxicity when the drug is administered with naproxen. When naproxen is administered with the anticoagulants there is an increased risk for bleeding.When naproxen is administered with the antihypertensives, there is a decrease in the antihypertensive effect.Coadministration of naproxen with the diuretics decreases the diuretic effect.
Rofecoxib
Rofecoxib is contraindicated in patients who are allergic to the drug, any of the NSAIDs, or the sulfonamides. The drug is not used during pregnancy (Category C) or lactation. Rofecoxib is used cautiously in patients with impaired renal or hepatic function, in those with a history of gastrointestinal bleeding or peptic ulcer disease, and in patients with congestive heart failure, asthma, or hypertension. Interactions with rofecoxib are similar to those with the other NSAIDs, such as an increased risk of bleeding when taken with anticoagulants and possible risk of lithium toxicity when taken concurrently with lithium.
ACTIONS
The NSAIDs are so named because they do not belong to the steroid group of drugs and thus do not possess the adverse reactions associated with the steroid and yet they have anti-inflammatory effects.In addition, NSAIDs have analgesic and antipyretic properties. Although the exact mechanisms of actions
are not known, the NSAIDs are thought to act by inhibiting prostaglandin (a group of naturally occur-ring fatty acids that act within the body to regulate acid secretion of the stomach, regulate body temperature and platelet aggregation, and control inflammation) synthesis by inhibiting the action of the enzyme cyclooxyge
nase, the enzyme responsible for prostaglandin synthesis. The NSAIDs act to inhibit the activity of two related enzymes:
1. cycloo1xygenase-1 (COX-1), the enzyme that helps to maintain the stomach lining; and
2. cyclooxygenase-2 (COX-2), the enzyme that
triggers pain and inflammation.
The anti-inflammatory effects of the NSAIDs are carried out by inhibition of COX-2. The gastrointestinal adverse reactions are caused by inhibition of COX
1. The newer NSAIDs (celecoxib and rofecoxib) appear to work by specifically inhibiting the COX-2
enzyme, without inhibiting the COX-1 enzyme.Celecoxib and rofecoxib relieve pain and inflamma-tion with less potential for gastrointestinal adverse reactions. The traditional NSAIDs, such as ibuprofen and naproxen, are thought to regulate the pain and inflammation by blocking COX-2. Unlike celecoxib and rofecoxib, these drugs also inhibit COX-1, the enzyme that helps maintain the lining of the stomach. This inhibition of COX-1 causes the unwanted gastrointestinal reactions, such as stomach irritation and ulcers.
USES
The NSAIDs have a variety of uses that vary depending on the drug selected. NSAIDs are used for the following conditions:
• Relief of signs and symptoms of osteoarthritis,rheumatoid arthritis, and other musculoskeletal disorders
• Mild to moderate pain relief
• Primary dysmenorrhea
• Fever reduction
ADVERSE REACTIONS
Many adverse reactions are associated with the use of the NSAIDs. However, many patients take these drugs and experience few, if any, side effects. Some of the adverse reactions associated with the use of these drugs are listed here.
• Gastrointestinal tract nausea, vomiting, diarrhea, constipation, epigastric pain, indigestion,abdominal distress or discomfort, intestinal ulceration, stomatitis, jaundice, bloating, anorexia, and dry mouth
• Central nervous system dizziness, anxiety, lightheadedness, vertigo, headache, drowsiness, insomnia, confusion, depression, and psychic disturbances
• Cardiovascular—congestive heart failure, decreaseor increase in blood pressure, and cardiac arrhythmias
• Renal—hematuria, cystitis, elevated blood urea nitrogen, polyuria, dysuria, oliguria, and acute renal failure in those with impaired renal function
• Special senses—visual disturbances, blurred or diminished vision, diplopia, swollen or irritated eyes, photophobia, reversible loss of color vision,tinnitus, taste change, and rhinitis
• Hematologic—neutropenia, eosinophilia, leukopenia, pancytopenia, thrombocytopenia, agranulocytosis, and aplastic anemia
• Skin—rash, erythema, irritation, skin eruptions,exfoliative dermatitis, Stevens-Johnson syndrome,ecchymosis, and purpura
• Metabolic/endocrinologic—decreased appetite,weight increase or decrease, hyperglycemia, hypoglycemia, flushing, sweating, menstrual disorders,and vaginal bleeding
• Other—thirst, fever, chills, and vaginitis
CONTRAINDICATIONS, PRECAUTIONS,
AND INTERACTIONS
The NSAIDs are contraindicated in patients with known hypersensitivity. There is a cross-sensitivity to
other NSAIDs. Therefore, if a patient is allergic to one NSAID, there is an increased risk of an allergic reaction with any other NSAID. Hypersensitivity to aspirin is a contraindication for all NSAIDs. In general, the NSAIDs are contraindicated during the third trimester of pregnancy and during lactation.
The NSAIDs are used cautiously in patients with bleeding disorders, renal disease, cardiovascular disease, or hepatic impairment and in the elderly. There is an increased risk of ulcer formation in patients older
than 65 years. Most NSAIDs are classified as Pregnancy Category B. In general, the NSAIDs are
used with extreme caution during pregnancy, especially in large doses or during the third trimester (see
above).
The NSAIDs prolong bleeding time and increase the effects of anticoagulants, lithium, cyclosporine, and the
hydantoins. These drugs may decrease the effects of diuretics or antihypertensive drugs. Long-term use of
the NSAIDs with acetaminophen may increase the risk of renal impairment.
COMMON ADVERSE REACTIONS
OF SELECT NSAIDs
Celecoxib
The most common adverse reactions seen with cele-coxib include dyspepsia, abdominal pain, diarrhea, nau-sea, and headache. Like other NSAIDs, celecoxib may compromise renal function. Elevation of aminotrans-ferase levels also occurs.
Ibuprofen
This drug is available to individuals as an over-the-counter drug and may be purchased without a prescrip-tion. The drug is used in children with juvenile arthritis and for fever reduction in children 6 months to 12 years.
Common adverse reactions seen with ibuprofen include headache, dizziness, somnolence, nausea, dyspepsia, gas-trointestinal pain, and rash.
Naproxen
Common adverse reactions seen with naproxen include headache, vertigo (dizziness), somnolence, insomnia,nausea, dyspepsia, gastrointestinal pain, and rash.
Rofecoxib
Common adverse reactions seen with rofecoxib includeheadache, dizziness, somnolence, insomnia, dyspnea,hemoptysis, and rash.
CONTRAINDICATIONS, PRECAUTIONS
AND INTERACTIONS
Celecoxib
Celecoxib is contraindicated in patients who are allergic to the drug itself, the sulfonamides, other NSAIDs, or aspirin; it also is contraindicated during pregnancy (Category C) and lactation.
The drug is used cautiously in patients with a history of peptic ulcer, individuals older than 60 years, and those taking an anticoagulant or steroids. In rare instances, serious stomach problems such as bleeding can occur without warning. When celecoxib is given with the anticoagulants, there is an increased risk for
bleeding.
Ibuprofen
Ibuprofen is contraindicated in individuals who are allergic to the drug or other NSAIDs; those who have hypertension, peptic ulceration, or gastrointestinal bleeding; and during pregnancy (Category B) and lacta-tion. The drug is used cautiously in patients with renal or liver dysfunction. When ibuprofen is used with
lithium, there is an increased risk of lithium toxicity. A decreased effect of the diuretic may occur when admin-istered with ibuprofen.When ibuprofen is administered with the beta-adrenergic blocking drugs there is a risk for a decrease in the antihypertensive effect of the beta-adrenergic blocking drug.
Naproxen
Naproxen is contraindicated in patients who are allergic to the drug or other NSAIDs and during pregnancy (Category B) and lactation. The drug is used cautiously in patients with asthma, hypertension, cardiac problems, peptic ulcer disease, and impaired liver or kidney function. Like ibuprofen, naproxen increases the risk of lithium toxicity when the drug is administered with naproxen. When naproxen is administered with the anticoagulants there is an increased risk for bleeding.When naproxen is administered with the antihypertensives, there is a decrease in the antihypertensive effect.Coadministration of naproxen with the diuretics decreases the diuretic effect.
Rofecoxib
Rofecoxib is contraindicated in patients who are allergic to the drug, any of the NSAIDs, or the sulfonamides. The drug is not used during pregnancy (Category C) or lactation. Rofecoxib is used cautiously in patients with impaired renal or hepatic function, in those with a history of gastrointestinal bleeding or peptic ulcer disease, and in patients with congestive heart failure, asthma, or hypertension. Interactions with rofecoxib are similar to those with the other NSAIDs, such as an increased risk of bleeding when taken with anticoagulants and possible risk of lithium toxicity when taken concurrently with lithium.
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Unknown - Thursday, 22 April 2010
